432-86-0

Upstream product

• 887144-94-7 Togni's reagent II 
• 13329-40-3 4-Iodoacetophenone 
• 2926-29-6 Langlois reagent 
• 99-92-3 p-aminobenzophenone 
• 458-99-1 (4-ethylphenyl)(trifluoromethyl)sulfane 
• 31218-75-4 (4-ethylphenyl)(methyl)sulfane 
• 432-85-9 1-ethyl-4-(trifluoromethylsulfonyl)benzene 

Downstream Products

• 609-66-5 2-chlorobenzamide 
• 731-09-9 2-methyl-4-(4-trifluoromethanesulfonyl-phenyl)-thiazole 
• 788-84-1 4-(4-trifluoromethanesulfonyl-phenyl)-thiazol-2-ylamine 
• 3829-16-1 3-ethyl-5-{2-[3-ethyl-4-(4-trifluoromethanesulfonyl-phenyl)-3H-thiazol-2-ylidene]-ethylidene}-2-thioxo-thiazolidin-4-one 

Relevant academic research and scientific papers

Method for constructing fluorine-containing methyl sulfone compound through multi-component coupling

The invention discloses a fluorine-containing methyl sulfone compound as shown in a formula (1) and a synthesis method thereof. Aromatic iodide (aryl iodide or heteroaryl iodide), an inorganic sulfur reagent and a fluorine-containing building block are used as reaction raw materials and react in a solvent under the action of alkali, a catalyst and an additive to obtain a series of fluorine-containing methyl sulfone compounds. According to the invention, the fluorine-containing sulfone compound is constructed by a one-pot two-step method by taking an inorganic sulfur reagent as a sulfur source under a catalytic condition, so that the defects of the traditional synthesis of a fluorine-containing sulfone compound by thioether oxidation are avoided. According to the synthesis strategy developed by the invention, some clinical methyl sulfone drugs can be modified, and monofluoro, difluoro and trifluoromethyl sulfone compounds can be successfully obtained, which have huge potential in the field of drug development in the future.

Rational Design and Development of Low-Price, Scalable, Shelf-Stable and Broadly Applicable Electrophilic Sulfonium Ylide-Based Trifluoromethylating Reagents

The development of two highly reactive electrophilic trifluoromethylating reagents (trifluoromethyl)(4-nitrophenyl)bis(carbomethoxy)methylide (1g) and (trifluoromethyl)(3-chlorophenyl)bis(carbomethoxy)methylide (1j) through structure-activity study was described. Under mild conditions, reagent 1g reacted with β-ketoesters and silyl enol ethers to give α-trifluoromethylated-β-ketoesters or α-trifluoromethylated ketones in high yields. In addition, reagent 1g could serve as a trifluoromethyl radical for a variety of trifluoromethylative transformations under visible light irradiation, including radical trifluoromethylation of electron-rich indoles and pyrroles and sodium aryl sulfinates as well as trifluoromethylative difunctionalization with styrene derivatives. On the other hand, as a complimentary, under reductive coupling conditions, reagent 1j reacted with a variety of (hetero)aryl iodides for the formation of trifluoromethylated (hetero)arenes.

Copper-Promoted Trifluoromethanesulfonylation and Trifluoromethylation of Arenediazonium Tetrafluoroborates with NaSO2CF3

A tunable chemoselective trifluoromethanesulfonylation and trifluoromethylation of arenediazonium tetrafluoroborates with Langlois' reagent (NaSO2CF3) was developed. The Cu2O-catalyzed reaction in DMSO gave aryl trifluoromethanesulfones as the major products. On the other hand, the trifluoromethylated arenes were produced in the presence of oxidant tert-butyl hydroperoxide, CuBF4(MeCN)4, and 2,2′;6′,2 terpyridine (tpy). Both of these transformations proceed under mild conditions and tolerate functional groups.